Plural Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/80)
  • Patent number: 10214768
    Abstract: The present application relates to new coumarin compounds and their uses as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: February 26, 2019
    Assignee: Illumina Cambridge Limited
    Inventor: Nikolai Romanov
  • Patent number: 10087179
    Abstract: A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: October 2, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Rikki Peter Alexander, Gareth Neil Brace, Julien Alistair Brown, Mark Daniel Calmiano, Prafulkumar Tulshibhai Chovatia, Michael Deligny, Ellen Olivia Gallimore, Jag Paul Heer, Victoria Elizabeth Jackson, Boris Kroeplien, Malcolm MacCoss, Joanna Rachel Quincey, Yogesh Anil Sabnis, Dominique Louis Léon Swinnen, Zhaoning Zhu, Uwe Heinelt, Volkmar Wehner
  • Patent number: 10000487
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. For Formula IA and Formula IB compounds A1, A2, A3, A4, W1, W2, Y, X, R1, R2, R3, R4a, R4b, R5a, R5b, R6, R7, R8, R9, R9a, R9b, R10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: June 19, 2018
    Assignee: eFFECTOR Therapeutics, Inc.
    Inventors: Paul A. Sprengeler, Seigfried H. Reich, Stephen E. Webber, Justin T. Ernst
  • Patent number: 9593113
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-KB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: March 14, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: David S. Weinstein, Hua Gong, Michael G Yang, Zili Xiao
  • Patent number: 9242992
    Abstract: Crystal forms of (3R,4S)-7-hydroxymethyl-2,2,9-trimethyl-4-(phenethylamino)-3,4-dihydro-2H-pyrano[2,3-g]quinolin-3-ol that are excellent as a drug, and production methods thereof. Production methods include crystallizing (3R,4S)-7-hydroxymethyl-2,2,9-trimethyl-4-(phenethylamino)-3,4-dihydro-2H-pyrano[2,3-g]quinolin-3-ol from an acetate ester solvent, an aliphatic hydrocarbon solvent, a nitrile solvent, an aromatic hydrocarbon solvent, a ketone solvent or an ether solvent, and crystal forms obtained according to the methods.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: January 26, 2016
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Yasutaka Takada, Miyako Kamon, Shiro Kawahara, Yasuhiro Umeda
  • Patent number: 9138434
    Abstract: The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is cyano or the like; R2 and R3 are hydrogen or the like; R4 is C1-6 alkyl or the like; R5 is C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, cycloalkyl-C1-6 alkyl, aralkyl or the like; R6 and R7 are each hydrogen, C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, C1-6 alkoxy-C1-6 alkyl, R12R13N—C1-6 alkyl or the like, which exhibit potent dopamine D2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: September 22, 2015
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Nishimura, Hirotaka Teranishi, Masako Yoshida, Yasunori Ueno, Kiyoshi Kasai
  • Patent number: 9132129
    Abstract: The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: September 15, 2015
    Assignee: KATHOLIEKE UNIVERSITEIT LEUVEN
    Inventors: Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
  • Publication number: 20150065499
    Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 5, 2015
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Patent number: 8969373
    Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: March 3, 2015
    Assignee: Shanghai Tangrun Pharmaceuticals Co., Ltd.
    Inventor: Suoming Zhang
  • Patent number: 8962648
    Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: February 24, 2015
    Assignee: OncoTherapy Science, Inc.
    Inventors: Yusuke Nakamura, Yo Matsuo, Shoji Hisada, Feryan Ahmed, Raymond Huntley, Zohreh Sajjadi-Hashemi, David M. Jenkins, Robert B. Kargbo, Wenge Cui, Polivina Jolicia F. Gauuan, Joel R. Walker, Helene Decornez, Mahender Gurram
  • Patent number: 8952363
    Abstract: A new class of compounds containing aza-dibenzothiophene or aza-dibenzofuran are provided. The compounds may be used in organic light emitting devices giving improved stability, improved efficiency, long lifetime and low operational voltage. In particular, the compounds may be used as the host material of an emissive layer having a host and an emissive dopant, or as a material in an enhancement layer.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: February 10, 2015
    Assignee: Universal Display Corporation
    Inventors: Chun Lin, Alexey Borisovich Dyatkin, Zeinab M. Elshenawy
  • Patent number: 8946260
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Publication number: 20140356873
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Zhenjun DIWU, Jixiang LIU, Kyle GEE
  • Publication number: 20140343092
    Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
    Type: Application
    Filed: September 18, 2012
    Publication date: November 20, 2014
    Inventors: Simon N. Haydar, Brian Alvin Johns, Emile Johann Velthuisen
  • Patent number: 8884017
    Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Timo Fleβner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
  • Patent number: 8871782
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: October 28, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah C. Johannessen
  • Publication number: 20140315927
    Abstract: The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: Andrew Simon Bell, lain Brian GARDNER, Karl Richard GIBSON, David Cameron PRYDE, Florian Michel WAKENHUT
  • Publication number: 20140296272
    Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Dorothée Bardiot, Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
  • Patent number: 8846925
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: September 30, 2014
    Assignee: Life Technologies Corporation
    Inventors: Zhenjun Diwu, Jixiang Liu, Kyle Gee
  • Publication number: 20140243311
    Abstract: The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is cyano or the like; R2 and R3 are hydrogen or the like; R4 is C1-6 alkyl or the like; R5 is C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, cycloalkyl-C1-6 alkyl, aralkyl or the like; R6 and R7 are each hydrogen, C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, C1-6 alkoxy-C1-6 alkyl, R12R13N—C1-6 alkyl or the like, which exhibit potent dopamine D2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Application
    Filed: March 12, 2012
    Publication date: August 28, 2014
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Nishimura, Hirotaka Teranshi, Masako Yoshida, Yasunori Ueno, Kiyoshi Kasai
  • Publication number: 20140228320
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Patent number: 8802853
    Abstract: Arylalkenyl and aryalkynyl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: August 12, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Jason D. Bonk, Joseph F. Dellaria, Jr.
  • Patent number: 8785638
    Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: July 22, 2014
    Assignee: Katholieke Universiteit Leuven
    Inventors: Dorothée Bardiot, Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
  • Patent number: 8772311
    Abstract: This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumor activity and lower nervous system toxicity by structurally modification of the parent structure of ?-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumor medicines and medicines used in treatment of tumor diseases in combination of light or radiation therapy.
    Type: Grant
    Filed: June 2, 2004
    Date of Patent: July 8, 2014
    Assignee: Xinjiang Huashidan Pharmaceutical Research Co., Ltd.
    Inventors: Jialin Wu, Qi Chen, Rihui Cao, Fusheng Yu, Zihou Wang, Wenlie Peng
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Publication number: 20140163219
    Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
    Type: Application
    Filed: July 23, 2012
    Publication date: June 12, 2014
    Applicant: Shanghai Tangrun Pharmaceuticals, Co., Ltd.
    Inventor: Suoming Zhang
  • Patent number: 8735421
    Abstract: Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: May 27, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Jason D. Bonk, Joseph F. Dellaria, Jr.
  • Publication number: 20140128383
    Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 8, 2014
    Applicant: LABORATOIRE BIODIM
    Inventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
  • Publication number: 20140128481
    Abstract: The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.
    Type: Application
    Filed: October 23, 2013
    Publication date: May 8, 2014
    Applicant: SENOMYX, INC.
    Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy DAVIS, Vincent DARMOHUSODO, Melissa WONG, Victor Selchau
  • Patent number: 8697873
    Abstract: Imidazopyridine, imidazoquinoline, and imidazonaphthyridine compounds having an amide substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: April 15, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Larry R. Krepski, Joseph F. Dellaria, Jr., Daniel E. Duffy, David T. Amos, Bernhard M. Zimmermann, William H. Moser
  • Patent number: 8686148
    Abstract: The invention relates to a process for preparing new tiotropium salts, these new tiotropium salts as such, pharmaceutical formulations containing them and their use for preparing a medicament for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: April 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rolf Banholzer, Waldemar Pfrengle, Peter Sieger
  • Patent number: 8673932
    Abstract: Imidazo-containing compounds (e.g., imidazoquinolines, imidazonaphthyridines, and imidazopyridines) with an oxime substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: March 18, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Tushar A. Kshirsagar, David T. Amos, Joseph F. Dellaria, Jr., Philip D. Heppner, Scott E. Langer, Bernhard M. Zimmermann
  • Patent number: 8658666
    Abstract: Imidazoquinolines and imidazonaphthyridines with a substituent containing a functional group, e.g., an amide, sulfonamide, urea, or heterocyclyl group, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: February 25, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Michael J. Rice, Chad A. Haraldson, John F. Gerster, Joshua R. Wurst, Philip D. Heppner, Bryon A. Merrill, Tushar A. Kshirsagar
  • Publication number: 20140045872
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: NOVARTIS AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Publication number: 20140018357
    Abstract: The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Inventors: Geraldine C. Harriman, Ronald T. Wester, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Jeremy Robert Greenwood
  • Patent number: 8592446
    Abstract: The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition, their use as a medicament, especially for treating a treatment neurodegenerative or haematological disease or condition, and a pharmaceutical composition comprising the compounds.
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: November 26, 2013
    Assignee: Noscira, S.A.
    Inventors: Ana Martinez Gil, Ana Castro Morera, Miguel Medina Padilla, Jorge Sanchez-Quesada, Mercedes Alonso Cascon, Laura Rubio Arrieta, Esther Garcia Palomero, Paola Usan Egea
  • Patent number: 8546421
    Abstract: Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: October 1, 2013
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Brent R. Stockwell, Wan Seok Yang, Rohitha Sriramaratnam
  • Patent number: 8541438
    Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: September 24, 2013
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk, Matthew R. Radmer
  • Patent number: 8541437
    Abstract: The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2i is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH?CH—, or ethynyl group —C?C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.
    Type: Grant
    Filed: April 1, 2008
    Date of Patent: September 24, 2013
    Assignee: Alla Chem, LLC
    Inventors: Andrey Alexandrovich Ivashchenko, Alexandre Vasilievich Ivachtchenko, Sergey Yevgenievich Tkachenko, Evgueni Borisovich Frolov, Oleg Dmitrievich Mitkin, Dmitri Vladimirovich Kravchenko, Ilya Matusovich Okun, Nikolay Filippovich Savchuk, Yan Lavrovsky
  • Patent number: 8518964
    Abstract: The present invention provides inhibitors of kinases, specifically I?B kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-?B-mediated diseases.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: August 27, 2013
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Jean-Francois Truchon, Nicolas Lachance, Cheuk Lau, Yves Leblanc, Christophe Mellon, Patrick Roy, Elise Isabel, Ryan D Otte, Jonathan R Young
  • Publication number: 20130178459
    Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.
    Type: Application
    Filed: March 29, 2011
    Publication date: July 11, 2013
    Applicant: Oncotherapy Science, Inc.
    Inventors: Yusuke Nakamura, Yo Matsuo, Shoji Hisada, Feryan Ahmed, Raymond Huntley, Zohreh Sajjadi-Hashemi, David M. Jenkins, Robert B. Kargbo, Wenge Cui, Polivina Jolicia F. Gauuan, Joel R. Walker, Helene Decornez, Mahender Gurram
  • Patent number: 8481737
    Abstract: The citrate salt of (S)-4-(4-Chloro-phenyl)-1-{3-[7-(1-hydroxy-1-methyl-ethyl)-11H-10-oxa-1-aza-dibenzo[a,d]cyclohepten-5-ylidene]-propyl}-3,3-dimethyl-piperidin-4-ol, which may be used in pharmaceutical applications, is disclosed. The crystalline Citrate Salt, including particular single crystal forms and combinations of the single crystalline forms, are also discussed. Mixtures for forming the crystalline salts are discussed. As well, methods of producing the Citrate Salt, and crystalline forms thereof, and using such Citrate Salt, and crystalline forms thereof, in treating diseases associated with aberrant leukocyte recruitment, activation, or recruitment and activation are also discussed.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: July 9, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Carole Neves, Aurelia Chevalier, Pascal Billot
  • Publication number: 20130165471
    Abstract: Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R3, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a 2-substituted-thienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a 2-substituted-thienoquinolone to an animal suffering from a microbial infection.
    Type: Application
    Filed: December 21, 2012
    Publication date: June 27, 2013
    Applicant: Achillion Pharmaceuticals Inc.
    Inventors: Avinash Phadke, Jason Allan Wiles
  • Publication number: 20130129677
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: December 7, 2012
    Publication date: May 23, 2013
    Applicant: Siga Technologies, Inc.
    Inventor: Siga Technologies, Inc.
  • Publication number: 20130131070
    Abstract: Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.
    Type: Application
    Filed: October 30, 2012
    Publication date: May 23, 2013
    Inventor: John K. Buolamwini
  • Patent number: 8426437
    Abstract: The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: April 23, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Hugues Bienayme, Antoine Dumoulin, Serge Grisoni, Bachir Kaloun El, Stephane Poigny, Remi Rabot, Rachid Rahali, Eric Tam, Pascaline Klein, Karim Bedjeguelal, Houcine Rahali
  • Patent number: 8420815
    Abstract: The present disclosure relates to novel compounds that can be used as anti-cancer agents in the prostate cancer therapy. In particular, the invention relates to N-acyl derivatives of 2,3-dihydro-1H-pyrrolo[2,3-b]quinolines having the structural Formula (I), stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or pharmaceutically acceptable salt and/or solvate thereof. The meaning of R1 is independently selected from H; C1-C6 Alkyl, cyclo-Alkyl or iso-Alkyl substituents; R2 is selected from C1-C6 Alkyl, cyclo-Alkyl or iso-Alkyl; substituted or non-substituted, fused or non-fused to substituted or non-substituted aromatic ring, aryl or heteroaryl groups. The invention also relates to methods for preparing said compounds, and to pharmaceutical compositions comprising said compounds.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: April 16, 2013
    Assignee: U.S. Department of Energy
    Inventors: Andrei A. Gakh, Mikhail Krasavin, Ruben Karapetian, Konstantin A. Rufanov, Igor Konstantinov, Elena Godovykh, Olga Soldatkina, Andrey V. Sosnov
  • Publication number: 20130060037
    Abstract: A new class of compounds containing aza-dibenzothiophene or aza-dibenzofuran are provided. The compounds may be used in organic light emitting devices giving improved stability, improved efficiency, long lifetime and low operational voltage. In particular, the compounds may be used as the host material of an emissive layer having a host and an emissive dopant, or as a material in an enhancement layer.
    Type: Application
    Filed: September 6, 2012
    Publication date: March 7, 2013
    Applicant: Universal Display Corporation
    Inventors: Chun Lin, Bin Ma, Raymond Kwong, Alexey Borisovich Dyatkin, Wu Yonggang, Zeinab M. Elshenawy
  • Patent number: 8367695
    Abstract: The problem of the present invention is to provide a compound having a GR selective binding activity, which shows less action on other nuclear receptors such as progesterone receptor (PR), mineralocorticoid receptor (MR) and the like. The present invention provides a condensed tetrahydroquinoline compound represented by the following formula (I) wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof or a hydrate thereof.
    Type: Grant
    Filed: January 15, 2008
    Date of Patent: February 5, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masahiro Eda, Tomoko Kuroda, Keiichi Aritomo, Yoshiyuki Aoki, Satoshi Kaneko
  • Patent number: 8343993
    Abstract: Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: February 22, 2006
    Date of Patent: January 1, 2013
    Assignee: 3M Innovative Properties Company
    Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, George W. Griesgraber, Philip D. Heppner, Kyle J. Lindstrom